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Another small compound targeting IBAT has been
2022-09-17
Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause
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br Role of FPRs in regulating the
2022-09-17
Role of FPRs in regulating the inflammatory response Annexin I is a glucocorticoid-regulated protein possessing both pro- and anti-inflammatory activity that might be mediated, in part, by FPR activation [35]. Expressed in a variety of cell types, annexin I is particularly abundant in neutrophils
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Ning et al showed that LPC appeared to increase
2022-09-17
Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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In C elegans KDM A appears
2022-09-17
In C. elegans, KDM4A appears to be involved in H3K36me3 reduction on the X chromosome, suggesting that this protein has a relevant role in germ cell development (Figure 2A) (47). In addition, in HeLa cells, KDM4A is associated with the repression of the achaete-scute complex homologue 2 (ASCL2) gene
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The H R antagonist cimetidine
2022-09-17
The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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Utilization of fascinating properties such as
2022-09-17
Utilization of fascinating properties, such as localized surface plasmon resonance (LSPR), high fluorescent quantum yield, biocompatible nature, chromogenic and electrocatalytic functionality of several nanomaterials for histamine sensing is also quite evident where the nanomaterials have served as
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Procainamide HCl Second although HO expression in the stroma
2022-09-17
Second, although HO-1 expression in the stromal macrophages has been seen in the other cancer tissues [21], the impact of HO-1 expression on EAOC progression has not been explored. We have found that the CD163+ M2-like Procainamide HCl were HO-1+ in OE, but malignant transformation may be associate
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Our data demonstrate that cobas HCV s performance characteri
2022-09-16
Our data demonstrate that cobas HCV’s performance characteristics meet these requirements, making the assay useful in the management of therapy for chronic hepatitis C. We documented that cobas HCV has the requisite LOD, measureable range (15 − 1.0E + 08 IU/mL) and precision allowing for baseline HC
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As well as the above studies Meier and coworkers used
2022-09-16
As well as the above studies, Meier and coworkers used TUG-891, alongside omega-3 fatty acids, to show a potential role for FFA4 in inhibiting proliferation of DU145 prostate cancer cells [68]. Given that these cells express both FFA4 and FFA1 and the current view that TUG-891 may not be sufficientl
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As disclosed in our preceding paper medicinal
2022-09-16
As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, Streptomycin sulfate l
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Level of CD and other blood parameters
2022-09-16
Level of CD4 and other blood parameters in patients before and after intervention are presented in Table 2. The mean of the CD4+ level before treatment in the intervention and placebo groups was 161.5 ± 291.1 and 159.9 ± 337.4, respectively (P = 0.232), which increased after treatment in both groups
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apelin receptor The dramatic increase in the
2022-09-16
The dramatic increase in the development of EAAT inhibitors and substrates over the last several years can likely be attributed to a number of experimental advances. Firstly, the isolation of the individual EAAT clones allowed each subtype to be selectively examined in well-characterized expression
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We also demonstrated that inhibition
2022-09-16
We also demonstrated that inhibition of NAAG hydrolysis to suppress glutamate production through a GCPII inhibitor is a viable target for cancer therapy. GCPII is also known as N-acetyl-L-aspartyl-L-glutamate peptidase I (NAALADase I) or NAAG peptidase (Pinto et al., 1996), and its increased express
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NU 7026 Extensive pharmacological and structural analysis sh
2022-09-16
Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in NU 7026 14, 17, 20. Functionally identical to REMD-477, REMD2.59 is
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FXR agonists represent an attractive class of drugs for pati
2022-09-15
FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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